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R306465, formerly known as JNJ-16241199, is a novel and potent inhibitor of hydroxamate-based histone deacetylase (HDAC) with broad-spectrum antitumour activity against solid and haematological malignancies in preclinical models.
| ln Vitro |
JNJ-16241199's effect on leukemia (ALL), acute myeloid leukemia (AML), chronic myeloid leukemia (CLL), chronic myeloid leukemia (CML), acute, and myeloma cell proliferation (IC50 = 15). JNJ-16241199 inhibits primary human mammary epithelial cells' proliferation with an IC50 value of 32 nM, while being insensitive to HMEC cells that are at rest and not actively proliferating (IC50 value of 7815 nM) [1]. -486 nanometers) [1]. In A2780 cells, -16241199 (0.1, 0.3, 1 μM, 24-48 h) can both stimulate and inhibit angiogenesis [1].
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| ln Vivo |
In orthotopic xenograft tumor models of A2780 ovarian cancer, H460 lung cancer, and HCT116 cancer, JNJ-16241199 (10–40 mpk daily for 28 days, po) suppresses the growth of tumors [1].
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| Cell Assay |
Cell cycle analysis [1]
Cell Types: human ovarian cancer cell A2780 Tested Concentrations: 0, 0.1, 0.3, 1 μM Incubation Duration: 24 hrs (hours) or 48 hrs (hours) Experimental Results: At 300 nM, the S phase diminished and the G1 phase increased in parallel, but after 24 hrs (hours) The sub-G1 fraction of cells increased at 1 μM. After 48 hrs (hours), there was an increase in the sub-G1 phase at all active concentrations starting from 100 nM. |
| Animal Protocol |
Animal/Disease Models: Human A2780, H460 and HCT116 orthotopic xenograft tumor model [1]
Doses: 10-40 mpk/day for 28 days Route of Administration: po (oral gavage) Experimental Results: Induction of H3 in A2780 ovarian tumor tissue Acetylation and p21waf1, cip1 promoter activity. Tumor volume reduction in three orthotopic xenograft tumor models. In the human A2780 orthotopic xenograft tumor model, the final tumor volume was diminished to a maximum of 76-87%. |
| References | |
| Additional Infomation |
R306465 has been used in trials studying the treatment of Neoplasms.
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| Molecular Formula |
C19H19N5O4S
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|---|---|
| Molecular Weight |
413.45026
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| Exact Mass |
413.115
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| CAS # |
604769-01-9
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| PubChem CID |
10309899
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Index of Refraction |
1.689
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| LogP |
2.06
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
29
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| Complexity |
669
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(C1=CN=C(N2CCN(S(=O)(C3=CC=C4C=CC=CC4=C3)=O)CC2)N=C1)NO
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| InChi Key |
MUTBJZVSRNUIHA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H19N5O4S/c25-18(22-26)16-12-20-19(21-13-16)23-7-9-24(10-8-23)29(27,28)17-6-5-14-3-1-2-4-15(14)11-17/h1-6,11-13,26H,7-10H2,(H,22,25)
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| Chemical Name |
N-hydroxy-2-(4-(naphthalen-2-ylsulfonyl)piperazin-1-yl)pyrimidine-5-carboxamide
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| Synonyms |
R 306465 JNJ-16241199R306465 JNJ16241199 R-306465JNJ 16241199.
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4187 mL | 12.0934 mL | 24.1867 mL | |
| 5 mM | 0.4837 mL | 2.4187 mL | 4.8373 mL | |
| 10 mM | 0.2419 mL | 1.2093 mL | 2.4187 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00677001 | COMPLETED | Drug: R306465 | Neoplasms | Johnson & Johnson Pharmaceutical Research & Development, L.L.C. | 2005-09 | Phase 1 |
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